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Chlordiazepoxide¿¡ ´ëÇÑ µ¶¼ºÁ¤º¸ : Á¤º¸º¸±â
Ãâó: ±¹¸³µ¶¼º°úÇпø µ¶¼º¹°ÁúÁ¤º¸DB : http://www.nitr.go.kr/nitr/contents/m134200/view.do |
| Mechanism of Action |
Chlordiazepoxide¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Chlordiazepoxide binds to stereospecific benzodiazepine (BZD) binding sites on GABA (A) receptor complexes at several sites within the central nervous system, including the limbic system and reticular formation. BZDs enhance GABA-mediated chloride influx through GABA receptor channels, causing membrane hyperpolarization. The net neuro-inhibitory effects result in the observed sedative, hypnotic, anxiolytic, and muscle relaxant properties.
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| Pharmacology |
Chlordiazepoxide¿¡ ´ëÇÑ Pharmacology Á¤º¸ Chlordiazepoxide has antianxiety, sedative, appetite-stimulating and weak analgesic actions. The precise mechanism of action is not known. The drug blocks EEG arousal from stimulation of the brain stem reticular formation. The drug has been studied extensively in many species of animals and these studies are suggestive of action on the limbic system of the brain, which recent evidence indicates is involved in emotional responses. Hostile monkeys were made tame by oral drug doses which did not cause sedation. Chlordiazepoxide revealed a "taming" action with the elimination of fear and aggression. The taming effect of chlordiazepoxide was further demonstrated in rats made vicious by lesions in the septal area of the brain. The drug dosage which effectively blocked the vicious reaction was well below the dose which caused sedation in these animals.
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| Metabolism |
Chlordiazepoxide¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 1A2 (CYP1A2)
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| Protein Binding |
Chlordiazepoxide¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Not Available
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| Half-life |
Chlordiazepoxide¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 24-48 hours
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| Absorption |
Chlordiazepoxide¿¡ ´ëÇÑ Absorption Á¤º¸ Not Available
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| Biotransformation |
Chlordiazepoxide¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic.
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| Toxicity |
Chlordiazepoxide¿¡ ´ëÇÑ Toxicity Á¤º¸ LD50=537 mg/kg (Orally in rats). Signs of overdose include respiratory depression, muscle weakness, somnolence (general depressed activity).
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| Drug Interactions |
Chlordiazepoxide¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Cimetidine Cimetidine increases the effect of the benzodiazepineClozapine Increased risk of toxicityEthotoin Possible increased levels of the hydantoin, decrease of benzodiazepineFosphenytoin Possible increased levels of the hydantoin, decrease of benzodiazepineMephenytoin Possible increased levels of the hydantoin, decrease of benzodiazepinePhenytoin Possible increased levels of the hydantoin, decrease of benzodiazepineFluconazole Fluconazole increases the effect of the benzodiazepineIndinavir The protease inhibitor increases the effect of the benzodiazepineRitonavir The protease inhibitor increases the effect of the benzodiazepineSaquinavir The protease inhibitor increases the effect of the benzodiazepineItraconazole The imidazole increases the effect of the benzodiazepineKetoconazole The imidazole increases the effect of the benzodiazepineVoriconazole The imidazole increases the effect of the benzodiazepineKava Kava increases the effect of the benzodiazepineNelfinavir The protease inhibitor increases the effect of the benzodiazepineOmeprazole Omeprazole increases the effect of benzodiazepine
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Food Interaction |
Chlordiazepoxide¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take without regard to meals.Avoid alcohol.
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| Description |
Chlordiazepoxide¿¡ ´ëÇÑ Description Á¤º¸ An anxiolytic benzodiazepine derivative with anticonvulsant, sedative, and amnesic properties. It has also been used in the symptomatic treatment of alcohol withdrawal. [PubChem]
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| Dosage Form |
Chlordiazepoxide¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Capsule Oral
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| Drug Category |
Chlordiazepoxide¿¡ ´ëÇÑ Drug_Category Á¤º¸ Adjuvants, AnesthesiaAnti-anxiety AgentsBenzodiazepinesGABA ModulatorsHypnotics and Sedatives
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| Smiles String Canonical |
Chlordiazepoxide¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CN=C1CN(O)C(C2=CC=CC=C2)=C2C=C(Cl)C=CC2=N1
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| Smiles String Isomeric |
Chlordiazepoxide¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ C\N=C1CN(O)C(C2=CC=CC=C2)=C2C=C(Cl)C=CC2=N\1
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| InChI Identifier |
Chlordiazepoxide¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C16H14ClN3O/c1-18-15-10-20(21)16(11-5-3-2-4-6-11)13-9-12(17)7-8-14(13)19-15/h2-9,21H,10H2,1H3/b18-15-
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| Chemical IUPAC Name |
Chlordiazepoxide¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 7-chloro-4-hydroxy-N-methyl-5-phenyl-3H-1,4-benzodiazepin-2-imine
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